VX-745

ATP-competitive inhibitor of MAPK14

Structure

Information

Protein target names: MAPK14

Mechanism of action: ATP-competitive inhibitor

Recommended in-cell concentration:
50-100 nM

In Vitro Validations

Uniprot ID: Q16539
Target Class: Protein kinase
Target SubClass: CMGC
Potency: KD
Potency Value: 2.8 nM
Potency Assay: KD was determined in a kinase binding assay. The IC50 (0.009 uM) was determined using a spectrophotometric coupled-enzyme assay.
PDB ID for probe-target interaction (3D structure): 3FC1
Target aliases:
Mitogen-activated protein kinase 14, SAPK2A, MXI2, ...

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is a selective probe with some off-target activity against p38β; it is able to cross the blood-brain barrier.

(last updated: 23 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This probe has a pretty good selectivity towards p38alpha with effects on peripheral blood mononuclear cells (PBMCs) and on a rheumatoid arthritis mouse model.

(last updated: 1 Jul 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Effective inhibition of p38α should be achievable at concentrations between 50-100 nM. The reported Ki for p38β is 220 nM as determined in α spectrophotometric coupled-enzyme assay using recombinant protein. The Kd for other kinases such as DDR1 is reported to be above 1000 nM.

(last updated: 3 Jul 2017 )

SERP Comments:

This compound is a fairly selective p38 MAPKα inhibitor with a 20-fold window to p38 MAPKβ based on assessement in an activity assay. It is also useful as an in vivo probe.

(last updated: 5 Jul 2017 )